Preparation, inhibiting peroxide oxidation of lipids

FIELD: chemistry.

SUBSTANCE: claimed is the application of 5(6)-nitro-2-chloro-benzimidazole of formula (I) as the preparation, inhibiting peroxide oxidation of lipids.

EFFECT: achievement of the claimed purpose, activity of the said formula compound is higher than of the comparison medication dibazole.

1 dwg

 

The present invention relates to organic chemistry and medicine, namely to the use of 5(6)-nitro-2-chloro-benzimidazole as a means of inhibiting lipid peroxidation (LPO).

As the agents involved in the inhibition of PAUL, known drugs such as vitamin E (α-tocopherol), vitamin C (ascorbic acid), β-carotene, the enzyme superoxide dismutase, as well as BHT (2,6-di-tert-butyl-4-METHYLPHENOL) and Mexidol (2-ethyl-6-methyl-3-hydroxypyridine succinate) [the State register of medicines, vol. 1. M., 2004, p. 103, 123, 142, 203, 290].

As a prototype and comparison drug taken Dibazol: 2-(Phenylmethyl)-1H-benzimidazol as the closest analogue of the chemical structure used in medical practice [Register of medicines [Electronic resource]. - Access mode: http://www.reles.ru/cat/drugs/Bendazil/. Reference date: 07.05.2014].

The object of the invention is to expand the Arsenal of biologically active substances, including having the property to inhibit the FLOOR.

The technical result - obtaining biologically active substances, inhibitory PAUL, as a means of inhibiting lipid peroxidation.

Summary of the invention the use of 5(6)-nitro-2-chloro-benzimidazole of the formula (I):

Synthesis of 5(6)-nitro-2-chloro-benzimidazole carried out by the method�e [Synthesis and biological activity of 5,6-dinitropropane benzimidazole / Chernova E. J., G. Mokrushina, A., Chupakhin O. N. etc. / / Chem.-Pharm. log. - 1991. - No. 1. - P. 50-53].

Assessment of the lower level FLOOR

The effect of the claimed compounds and product comparison on the processes of free radical oxidation (fro) in model systems in vitro was studied using a rapid method for determination of antioxidant activity, based on the detection of chemiluminescence (CHL) - the glow arising from the interaction of free radicals [Farkhutdinov P. P. of research Methodology chemiluminescence of biological material on chemiluminometer CL - 003. / Farkhutdinov P. P., S. I. Tevdoradze // Methods for evaluation of antioxidant activity of biologically active substances of therapeutic and prophylactic purposes: Sat. Dokl. nauch.-practical. of the seminar. - M., 2005. - P. 147-154]. Registration of luminescence was carried out on the device "HL-003" Russia. CL model systems were characterized by spontaneous glow, fast flash, and then a slow-paced flash. The most informative characteristics of CL were the sum of the luminescence is determined by the radiation intensity, and amplitude maximum luminescence. To assess the impact on the processes of SRO in vivo studies were carried out on model systems in which the flow of the reaction FLOOR. The influence of the studied compounds on PAUL studied in the chicken yolk lipids, similar in composition to Lee�Itami blood. Lipids were obtained by homogenization of chicken yolk in phosphate buffer in the ratio 1:5 and then diluted 20-fold, were selected by Adding 10 ml. in 1 ml of 50 mm solution of Fe2+led to the initiation of the oxidation of unsaturated fatty acids, which was accompanied by chemiluminescence. The illumination intensity was judged on the process FLOOR. Drugs were added to the model system at concentrations corresponding to therapeutic dose prescribed drugs Dibazol. As control was used a model system in which instead of the test preparations were added to 0.9% saline in the same volume.

The invention is illustrated in the drawing, which shows the effect of the claimed compounds and Dibazol on the SRO processes in the model system of lipid peroxidation, where To control, I - the claimed compound II - product comparison Dibazol.

In the model system of liposomes tested compound inhibited the spontaneous level of illumination, reduced flash and the CL light sum (drawing). Thus, the antioxidant activity of compound (I) induced when the FLOOR is higher than the reference drug - Dibazol.

The use of 5(6)-nitro-2-chloro-benzimidazole of the formula

as a means of inhibiting lipid peroxidation.



 

Same patents:

FIELD: medicine.

SUBSTANCE: method for preparing an agent possessing anti-inflammatory, diuretic and antioxidant activity, involving milling Spiraea salicifolia shoots representing a mixture of leaves, blossom and shoots, extracting them three times by gradual maceration, mixing in infusing, filtering, condensing, separating, drying in the certain environment.

EFFECT: agent shoes the pronounced anti-inflammatory, diuretic and antioxidant activity.

2 dwg, 12 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and can be used as a hepatotrophic, lipotropic agent in gastroenterology, as well as for treating cardiac and cerebral atherosclerosis, in neurology in the lower extremity artery diseases (endarteritis). The agent contains tabletted powders of diisopropylammonium dichloroacetate, microcrystalline cellulose, lactose and excipients presented by Aerosil, Primogel and calcium stearyl fumarate.

EFFECT: agent possesses no toxicity, has the high adsorption properties, the apparent anti-inflammatory action, and provides metabolism and the liver regeneration.

3 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to heterocyclic compound - 6-methyl-5-morpholynomethyl-1-(thiethan-3-yl)pyrimidine-2,4(1H,3H)-dione of formula 6-methyl-5-morpholynomethyl-1-(thiethan-3-yl)pyrimidine-2,4(1H,3H)-dione of formula: .

EFFECT: novel compound, possessing antioxidant activity, is obtained.

2 cl, 6 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, and concerns a pharmaceutical composition for treating gastroduodenal ulcer in the form of tablets, capsules or gel, containing therapeutic agents and a consistency base applicable for each dosage, wherein the therapeutic agents are as follows: recombinant interferon specified in a group: recombinant interferon alpha, recombinant interferon beta, recombinant interferon gamma; antiseptics; amino acids specified in a group: arginine, histidine, lysine, cysteine, methionine, glutamic acid; and antioxidants specified in a group: beta-carotene, vitamin C, vitamin E.

EFFECT: invention has the integrated body effect promoting faster healing of the mucosal defect accompanying the aggravated gastroduodenal ulcer and preventing recurrences, including by the eradication effect.

6 cl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, and concerns a pharmaceutical composition in the form of tablets for oromucosal administration in treating infectious-inflammatory oropharyngeal diseases. The composition contains recombinant interferon specified in a group: recombinant interferon alpha, recombinant interferon beta, recombinant interferon gamma; amino acid specified in a group: arginine, histidine, glycine, glutathione, lysine, methionine, cysteine; an antiseptic, a preserving agent, flavours specified in a group: tea tree oil, eucalyptus leaf oil, mint leaf oil and a consistence base.

EFFECT: invention makes the composition applicable in fragile and frequently ill patients for reducing a disease recurrence.

7 cl, 1 ex

FIELD: food industry.

SUBSTANCE: biologically active food additive strengthening the organism adaptive power and body defences and having anti-inflammatory and antioxidant activity contains vegetal origin components represented by a complex extract of devil's-club root, Rhaponticum carthamoides root, Hedysarum neglectum Ledeb root, celery roots and leaves, rhodiola rosea root, Japanese angelica tree roots, boschniakia rossica roots, Hungarian sainfoin herb, magnolia-vine fruits; additionally the additive contains chitosan, trepang fermentative hydrolysate, ascorbic acid, taurine, glutathione, nicotinamide, vitamin B1, vitamin B2, vitamin B6, vitamin B12, folic acid, anhydrous calcium chloride, magnesium chloride, zinc chloride, bee honey at preset ingredients ratio.

EFFECT: biologically active food additive promotes effective strengthening of the organism adaptive power and body defences and human aging retardation.

4 tbl, 6 ex

FIELD: medicine.

SUBSTANCE: invention relates to medical radiology and can be used for prevention of cerebral form of acute radiation sickness. Claimed is application of officinal drug pyrazinamide as medication for prevention of cerebral form of acute radiation sickness. Pyrazinamide has been used for treating tuberculosis.

EFFECT: preventing in 100% of cases development of early temporary incapacity in case of irradiation in dose 200 Gy, improvement of indices of behavioral and research activities in irradiated animals, in reduction of frequency of motor disorders, reduction of frequency and expression of convulsive-hyperkinetic syndrome and 9,5 fold increase of average life expectancy of irradiated animals Pyrazinamide is not inferior to drug - nicotinamide prototype in efficiency of radioprotective action.

4 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and represents a composition possessing the antioxidant and antibacterial activity and containing lithium ascorbate, differing by the fact that it additionally contains lithium benzoate in the following proportions, wt %: lithium ascorbate - 50; lithium benzoate - 50.

EFFECT: invention provides extending the range of antioxidants with antibacterial activity possessing normothymic activity.

1 ex, 2 tbl

FIELD: medicine.

SUBSTANCE: method for increasing the antitoxic body function in healthy individuals occupied in the chemical load environment involving administering an antioxidant water containing carrot juice, cod liver oil, olive oil, honey; the water is taken daily before the working shift for 10 days.

EFFECT: using the invention enhances the antitoxic body function by administering the water having high antioxidant properties.

1 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is described is using a pharmaceutical composition in the form of an orally disintegrated tablet containing 6-methyl-2-ethyl-3-hydroxypyridine succinate as an active substance and crospovidone as a disintegrating agent in ratio 2:1 respectively, as a motor stimulating and anorectic agent.

EFFECT: preparing motor stimulating and anorectic agent.

16 dwg, 34 tbl, 13 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry and represents method of medication encapsulation by precipitation with non-solvent, which is characterised by the fact that as medication used is fenbendazole, and as envelope - sodium carboxymethylcellulose, which is precipitated from solution in acetone by addition as non-solvent of methylcarbinol and water at 25°C.

EFFECT: invention ensures simplification and acceleration of process of obtaining microcapsules, reduction of loss in obtaining microcapsules (increase of output by weight).

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to an albendazole-based composition. The claimed composition consists of a substance of albendazole and arabinogalactane polysaccharide from Siberian larch or Gmelin with weight ratios of the components albendazole : arabinogalactane 1:5-20.

EFFECT: invention possesses the higher anti-opisthorchosis pharmaceutical activity than albendazole, and does not cause the toxic injury of hepatocytes.

3 cl, 7 dwg, 2 tbl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to encapsulation, particularly a method of producing fenbendazole microcapsules in a sodium carboxymethyl cellulose capsule. The method includes dissolving fenbendazole in dioxane or dimethyl sulphoxide or dimethyl formamide, adding the obtained fenbendazole solution to a solution of sodium carboxymethyl cellulose in tetrachloromethane in the presence of E472c while stirring at a rate of 1000 rps. Fenbendazole and sodium carboxymethyl cellulose are taken in weight ratio of 1:3. Methanol and distilled water, taken in ratio of 2:1 vol/vol, are then added. The obtained suspension of microcapsules is filtered and dried. The process is carried out at 25°C for 20 minutes.

EFFECT: invention simplifies and speeds up the process of producing microcapsules, reduces losses during production thereof (high mass output).

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry and represents method of medication encapsulation by precipitation with non-solvent, which is characterised by the fact that as medication used is fenbendazole, and as envelope - sodium carboxymethylcellulose, which is precipitated from solution in ethylacetate by addition as non-solvent of carbinol and water at 25°C.

EFFECT: invention ensures simplification and acceleration of process of obtaining microcapsules, reduction of loss in obtaining microcapsules (increase of output by weight).

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the chemical-pharmaceutical industry and represents a method of medication encapsulation by precipitation with a non-solvent, which is characterised by the fact that as the medication used is fenbendazole, and as an envelope - sodium carboxymethylcellulose, which is precipitated from a solution in diethyl ether by the addition as the non-solvent of carbinol and water at 25°C.

EFFECT: invention ensures the simplification and acceleration of the process of obtaining microcapsules, reduction of loss in obtaining the microcapsules (increase of output by weight).

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of encapsulation, in particular to a method of obtaining fenbendazole microcapsules in an envelope of sodium carboxymethylcellulose. In accordance with the method fenbendazole is dissolved in dioxane or dimethylsulphoxide, or dimethylformamide, the obtained fenbendazole solution is added to a solution of sodium carboxymethylcellulose in methanol in the presence of E472c with mixing at a rate of 1000 rev/s. Fenbendazole and sodium carboxymethylcellulose are taken in a weight ratio of 1:3. After that ethanol and distilled water, taken in a ratio of 2:1 vol/vol, are added. The obtained suspension of microcapsules is filtered and dried. The process is realised at 25°C for 20 minutes.

EFFECT: invention ensures the simplification and acceleration of the process of obtaining microcapsules, reduction of loss in their obtaining (increase of output by weight).

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the chemical-pharmaceutical industry and represents a method of medication encapsulation by precipitation with a non-solvent, which is characterised by the fact that as the medication used is fenbendazole, and as an envelope - sodium carboxymethylcellulose, which is precipitated from a solution in diethyl ether by the addition as the non-solvent of isopropanol and water at 25°C.

EFFECT: invention ensures the simplification and acceleration of the process of obtaining microcapsules, reduction of loss in obtaining the microcapsules (increase of output by weight).

3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of encapsulating fenbendazole. Said method is characterised by that fenbendazole is dissolved in dioxane or dimethyl formamide, then dispersed in a mixture of sodium carboxymethyl cellulose and butanol in the presence of E472c, followed by addition of isopropanol and water, and filtering and drying the obtained suspension of microcapsules.

EFFECT: method provides a simple and fast process of producing microcapsules and increases mass output.

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the chemical-pharmaceutical industry and represents a method of medication encapsulation by a method of precipitation with a non-solvent, characterised by the fact that as the medication used is fenbendazole and as an envelope sodium carboxymethylcellulose, which is precipitated from a solution in dicloromethane by the addition of carbinol as the non-solvent and water at 25°C.

EFFECT: invention ensures the simplification and acceleration of the process of obtaining microcapsules, reduction of loss in obtaining the microcapsules (increase of output by weight).

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the chemical-pharmaceutical industry and represents a method of medication encapsulation by a method of precipitation with a non-solvent, characterised by the fact that as the medication used is fenbendazole and as an envelope sodium carboxymethylcellulose, which is precipitated from a solution in toluene by the addition of isopropanol as the non-solvent and water at 25°C.

EFFECT: invention ensures the simplification and acceleration of the process of obtaining microcapsules, reduction of loss in obtaining the microcapsules (increase of output by weight).

3 ex

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to new derivatives of benzimidazole represented by the following formula (I) or its salt:

wherein R1 represents (lower)-alkyl group; R2 represents aromatic (lower)-alkyl group that can be substituted with one or more groups taken among halogen atom, alkyl group, halogen-(lower)-alkyl group, nitro-group, aromatic group, aromatic (lower)-alkoxy-group, (lower)-cycloalkyloxy-(lower)-alkyl group, aromatic (lower)-alkyl group, aromatic (lower)-alkenyl group, aromatic (lower)-alkynyl group, aromatic oxy-(lower)-alkyl group, (lower)-cycloalkyl-(lower)-alkoxy-group, alkenyl group, (lower)-alkoxy-group, (lower)-alkylthio-group and (lower)-alkanesulfonylcarbamoyl group; R3 represents alkyl group, hydroxy-(lower)-alkyl group, alkenyl group, aromatic group, halogenated aromatic group, (lower)-alkyl aromatic group, (lower)-alkenyl aromatic group or aromatic (lower)-alkenyl group; -X- represents cross-linking group represented by one of the following formulas: (II) , (III) , (IV) , (V) . Also, invention relates to pharmaceutical compositions eliciting activity that reduces blood glucose level based on this compound. Invention provides preparing new compounds and pharmaceutical compositions based on thereof used for prophylaxis and treatment of damaged tolerance to glucose, diabetes mellitus, insulin-resistance syndrome, vascular failures syndrome, hyperlipidemia and cardiovascular disorders.

EFFECT: valuable medicinal properties of compounds and compositions.

16 cl, 1 tbl, 86 ex

Up!